Composition for cosmetic, pharmaceutical or dietary applications

ABSTRACT

A composition including 0.5-40% vegetable extracts, 30-90% carbohydrate and 0.5-30% of phospholipid with 40-80% phosphatidylcholine for cosmetic, pharmaceutical or dietary uses.

This application is a continuation application filed under 35 U.S.C.§111(a) of International Application No. PCT/IB2009/052707, filed Jun.24, 2009, the entire contents of which are incorporated herein byreference.

FIELD OF THE INVENTION

The present invention is related to a composition comprising vegetableessence and/or ingredients and/or active agents, carbohydrate andphospholipid, a method for production of such a composition and thepharmaceutical, dietary or cosmetic application of such a composition.

BACKGROUND OF THE INVENTION

Vegetable resources are of continuously increasing importance for thepreparation of pharmaceutical, dietary or cosmetic applications. Thedemand for purely natural models is of increasing importance. Vegetableresources, particularly vegetable essences with active agents are notalways stable and in most of the cases difficult to insert into a model.

The document U.S. Pat. No. 5,387,415 discloses the production of Aloevera juice pellets by seeping said juice with with collagens into liquidazote at −196° C. The method is very onerous at high energy consumption.A similar method is taught in U.S. Pat. No. 5,401,502.

The document U.S. Pat. No. 5,387,415 discloses bisabolol nanoparticles,pre-emulsion with lecithin in a high pressure homogenizer, subsequentlyspray dried by means of starch and maltodextrin. It has always to beworked with a starch dye. The products are spray dried. Many vegetableextracts and their ingredients are very sensitive and may be decomposedor exhausted during spray drying. Said decomposition or exhaustion oughtto be avoided.

The document U.S. Pat. No. 5,180,713 discloses the production ofpharmaceutical liposomes in organic solvents in the presence ofcryoprotectants, such as sugar. It has to be worked in organic solvents,being difficult to remove from the end-product and being unwanted innatural products.

The document U.S. Pat. No. 6,534,087 discloses foamed pills of activeagents; lecithin and maltodextrin. Measured powders or granules withstable characteristics can't be produced like that.

The document US 20040234673 discloses a composition with an amorphouscarbohydrate phase, a crystalline phase and a third phase, selected fromone or more substances made of aroma, volatile substances and substancessensitive towards external impacts, the third phase being dispersed bymeans of emulsifiers in the other two phases. Any extrusion of thiscomposition is carried out at high temperatures. By working at highertemperatures the ingredients of the vegetable extracts are decomposedand their intended activity can not be provided.

The patent applications EP 209037, EP 209038, EP 275005, EP 275224, EP283713, EP 300282, EP 304603, EP 441279, EP 464297, EP 1390008, EP1837030, EP 1844785 disclose stabilization of vegetable extracts bycomplex formation of the active agents with phospholipids. For this workhas to be done in solvents, such as methylene chloride or methanol. Thismode of operation is very elaborate and requests the use of questionablesolvents.

The problems of formulation and the limited stability during transportand storage of the compositions of the state of the art are due to theselection of their components, particularly the quality of the lecithinswith shares of phosphatidylcholine of less than 15%.

SUMMARY OF THE INVENTION

The object of the present invention is therefore to provide acomposition with a high share of vegetable extracts and/or ingredientsand/or active agents, with a high stability during transport and storageand easily and gently to work to formulations. It is a further object ofthe invention to provide a method for the production of such acomposition and suitable applications for such a composition.

The inventive compositions contain 0.5-40% of vegetable extract and/orvegetable active agents, 10-90% of a carbohydrate and 0.5-30% of aphospholipid. Preferred are compositions with 18-35% of vegetableextract and/or vegetable active agents, 40-80% carbohydrate and 1-25%phospholipids. Particularly preferred are compositions with 30% ofvegetable extract and/or vegetable active agents, 67% carbohydrate and3% phospholipids. The compositions allow high shares of active agents inthe formulations. The compositions are free of conservation-means andsolvents and consist mostly of natural vegetable resources.

Vegetable resources may be extracts from plants or parts of plants,fruit concentrates, herbs extracts, vegetable oils and alike, such asAcai-extract (Euterpe oleracea), Acerola extract (Malpighia glabra),Field Horsetail (Equisetum arvense), Agarius extract (Agarius blazeimurill), Aloe (Aloe vera, Aloe Barbadensis), Apple extract (Malus),Artichoke leave extract (Cynara scolymus), Artichoke flower extract(Cynara edulis), Arnica (Arnica Montana), oysters extract, Ostreaedulis), valerian root extract (Valeriana officinalis), bearberry leaveextract (Artostaphylos uva-ursi), bamboo extract (Bambus vulgaris,Bamboo), Bitter melon extract (Momordica charantia), Bitter orangeextract (Citrus aurantium), Nettle leave extract (Urtica dioica),Nettle-root-extract (Urtica dioica), Broccoli extract (Brassicaoleracea), Water cress (Rorippa nasturtium), Painted Nettle extract(Coleus forskohlii), Capsicum extract (Capsicum frutescens), Centellaasiatica (Gotu Kola), Cinchona extract (Cinchona), Cranberry extract(Vaccinium vitis-daea), Curcuma extract (Curcuma longa), Damiana extract(Tunera diffusa), Red Pitaya extract (Pitahaya), Echinacea Purpurea,wheaten Placenta extract, Edelweiss extract (Leotopodium alpinum), Ivyextract (Hedera helix), Earth-root-spine extract (Tribulus terrestris),Garcinia Cambogia extract (Garcinia Cambogia), Ginkgo extract (Ginkgobiloba), Ginseng extract (Panax ginseng), Pomegranate extract (Punicagranatum), Grapefruit extract (Citrus paradisi), Griffonia extract(Griffonia simplicifolia), Green tea extract (Camellia sinensis),Guarana extract (Paullinia cupana), cucumber extract (Cucumis sativus),Rose hip extract (Rosa canina), Blueberry extract (Vaccinium myrtillus),Hibiskus extract (Malvacea, Malvenextrakt), Honey extracts, Hop extract(Humulus), Ginger extract (Zingiber officinale), Iceland Moss (Ceterariaislandica), Jojoba extract (Simmondsia chinensis), St. Johns Wort,(Hypericum Perforatum), Coffee concentrate, Cacaobeans extract(Theobroma cacao), Cactusflower extract, Chamomile flower extract(Matricaria recutita, Chamomile, Matricaria Chamomila), Carrot extract(Daucus carota), Kiwi extract (Aperygidae), Kudzu extract (Puerarialobata), Coconut milk extract, Pumpkin seed extract (Curcurbita pepo),Cornflower extract (Centaurea cyanus), Lotus extract, Dandelion rootextract (Taraxacum officinale), Maca extract (Lepidium peruvianum),Magnolia flower extract, Mango extracts, Holy thistle extract (Silybummarianum), Marie gold (Calendula Officiennalis), Mate extract (Ilexparaguariensis), Butcher's broom extract (Rugcus aculeatus), Sea algaextracts, Cranberry, (Kraanbeere, Vaccinium macrocarpon), MoringaOleiferaextrakt, Musk Mallow (Malva moschata), Evening primrose oilextract (Azadirachta indica), Nettle extract (Urticaceae), Olive leaveextract (Olea europea), Orange extract (Hespridin), Orchide extract,Papaya extract (Carica papaya), Peppermint extracts, Carica papaya(Geissospermum), Sour Orange extract (Citrus aurantioum), Cowberryextract (Vaccinium vitas-ideea), Pygeum Afrikanum extract (Prunusafricana), Herbasec extracts, Resveratrol extract (Polygonumcuspidatum), Rooibos (Aspalasthus Linnearis), Rose hip extract, Horsechestnut extract (Aesculus hippocastanum), Rosmary, (RosemarinusOfficinalis), Red clover extract (Trifolium platense), Red wine extract(Vitis vinifera), Saw Palmetto extract (Serenoa repens), Salade extract(Lactuca sativa), Sandal-wood extract (Santalum rubrum), Sage, (SalviaOfficinalis), Horsetail extract (Equisetum), Milfoil (Achilleamillefolium), Black Pepper extract (Piper nigrum), Black tea extract,Water lily extract (Nymphaea), White Willow, (Willow Bark, Salix Alba),Licorize (Glycyrrhiza), Rampion root extract (Harpagophytum procumbens),Thyme extract (Thymus vulgaris), Tomato extract (Lycopersicumesculentum), Grapeseed extract (Vitis vinifera), Grape peel extract(Vitis vinifera), Rorippa amphibia, Willow bark-extract (Salix alba),Incense extract (Artemisia absinthium), White tea extract, Yam extract(Dioscorea opposita), Yohimbin extract (Pausinystalia yohimbe), Witchhazel (Hamamelis), Cinnamon extract (Cinnamomum cassia Presl), Lemonextract (Citrus), Onion extract (Allium cepa).

Vegetable active agents or ingredients may be used apart from theextracts alone or in combination. Vegetable active agents may be:glycyrrhizin, coffein, proanthocianidin, hesperitin, rutin, luteolin,polyphenols, aspalatin, oleuropin, theobromin, bioflavanoids orcombinations of glycyrrhizin and Glycerica glabra extracts, coffein undCamellia sinesis or Camellia alba or Guarana (Paulinia cubana) or Coffesarabica, proanthocianidin and Vitis vinifera (Vine), hespiridin andrutin und Citrus aurantii amara peel extract, luteolin and Chamomillareticulataq, polyphenols and Camellia sinensis or Vaccinium macrocarpon(Cranberry), coffein/theobromin and Ilex paraguaiensis (Mate),bioflavanoids and Green tea extract (Camellia sinensis), Curcumin andCurcuma longa, epigallocatechingallate, catechin, epicatechine,narginin, hesperidin, neohesperidin, asiaticiside, ellagitannin,chlorogen acid, oleuropei, arbutin, betuli, esculin, sylimarin, etc.,particularly isoflavone puerin (from or with Pueraria lobata extract),oleuropein (from or with Olea europea Leaf extrakt), luteolin (from orwith Chamilla reticulate), Baicalin (from or with Scutellariabalcalinensis Rott extract), Chorogenic acid (from or with Eucommiaulmoides/Guttapercha tree extract), apigenin (from or with Citrusgrandis peel extract), hesperidin (from or with Citrus aurantium amarapeel extract), coffein (from or with Paulinia cubana/Guarana extract),aspalatin (from or with Aspalatus linnearis/Rooibos extract), rutin(from or with Sophora japonica extract), polyphenol, quinic acid (fromor with Vaccinium marcrocarpon/Cranberry extract), allagitannins (fromor with Punica granatum/Pomegranate extract), Asiaticoside (from or withCentella asiatica extract), proanthocianidine (from or with Vitisvinifera extract (Proanthocianidine), rutin (from or with Viola odorataextrakt), 18 beta Glycyrrhetic acid (from or with Liquiritia extract),Glycyrrhizin (from or with Liquiritia extract), theanin, polaphenols(from or with Camellia/Thea sinsnesis extract), coffeolychinic acid,caffeine, theobromone (from or with Ilex paraguaiensis/Mate extract).

Phospholipids may be phospholipids and phospholipid-fractions ofvegetable resources, such as from soya beans, Sunflowers, Rape, peanut,corn, Lupines or cotton seed or egg yolk phospholipids with a share ofphosphatidylcholine of 20-100%. Or defined phospholipids such asDi-acyl-phosphatidylcholine (e. g. Dimyristoyl-, Dipalmitoyl-,Disteraoyl-phosphatidylcholine), hydrated phospholipids, hydrolized ormodified phospholipids. Phospholipid-fractions are preferred with ashare of phosphatidylcholin of 40-80%.

Lecithin is composed of neutralipids, glycolipids and phospholipids. ThePhospholipids are composed of e. g. phosphatidylcholine (PC),phosphatidylethanolamin (PE), phosphatidylinositol (PI),phosphatidylserin (PS), lysophosphatidylcholine (LPC),lysophosphatidylethanolamine (LPE), lysophosophatidylinositol (LPI) usw.(A. Wendel Lecithin, Kirk-Othmer Encyclopedia of Chemical Technology,Fourth Edition, Volume 15; Willem van Nieuwenhuyzen, Fett/Lipid 99(1997, Nr. 1, S10-14, Willem van Nieuwenhuyzen, Eur. J. Lipid Sci.Technol 2008, 110, 472-486. Customary lecithin contains about. 12-15%phosphatidylcholine. De-oiled lecithin, as well called pure lecithin,contains 20-25% phosphatidylcholine. Phospholipid-fractions with sharesof 30 to 100% phosphatidylcholine may be produced by fractioning withethanol. Customary products enriched with phosphatidylcholine are e.g.phospholipids of soy as e.g. Lipoid S 20 (approx. 20-24% PC, 16-22% PE),Lipoid S45 (45% PC, 10-18% PE), Lipoid S75 (70% PC, 7-10% PE), LipoidS80 (75% PC, 7% PE), Lipoid S100 (>94% PC), phospholipon 20 (about20-24% PC, 16-22% PE), phospholipon 50 (approx. 45-50% PC), phospholipon85G (>80% PC), phospholipon 90G (>95% PC) or phospholipids of rape, suchas e. g. Lipoid R20 (approx. 20-24% PC, 16-22% PE), Lipoid R75 (70% PC,7-10% PE), Lipoid R45 (45% PC, 10-18% PE), Lipoid R75 (75% PC, 7% PE),Lipoid R80 (75% PC, 7% PE), Lipoid R100 (>94% PC) or soy phospholipidsfrom genetically non modified (non GMO) soy beans such as e. g. LipoidP45 (45% PC, 10-18% PE), Lipoid P75 (75% PC, 7% PE) , Lipoid P100 (>94%PC).

Sugar (mono-, di-, or polysaccharides) like manit (mannitol), glucose(dextrose), trehalose (mykose), saccharose (sucrose), lactose (milksugar), fructose (levulose), mannose, ribose, galactose, fructose,rhamnose, lactulose, maltose, raffinose, dextrin or maltodextrin areused for carbohydrates. Mannit, glucose, trehalose are preferred andparticularly preferred is maltodextrin.

The inventive composition is produced by dissolving or dispersing theelements simultaneously or subsequently at room temperature in water andby homogenizing in customary devices, such as for example by amicrofluidizer, 1-3 cycles, after that filtration or sterile filtration,e.g. by a 2-8 μm filter-candle and subsequently by freeze- orvacuum-drying gently at −30° C. to +45° C. The dried product may beground to the wanted grain size in suitable devices with an orificediameter of 0.5-1.5 mm.

Liposomal compounds may be produced at redispersing.

The dried composition is stable for transport and storage and easy towork into cosmetic, dietary and pharmaceutical formulations. Advantagesare the good solubility, the wettability of the active agent isimproved, the characteristics at dispersion of the active agents areoptimized, the stability of the active agent against environmentalimpacts is improved, odor and taste of the active agent is optimized.

During treatment of the new composition in cosmetic, dietary andpharmaceutical formulations the best bio-disposability is achieved.

Formulations are e. g. oral, such as powders, granules, pills, capsulesand topic preparations such as creams, lotions, etc. by adding thecustomary additives.

EXAMPLES Example 1

Aloe Vera 10 kg (10%) is mixed with 87 Kg (87%) maltodextrin and 3 kg(3%) Lipoid P45 and dispersed in 100 kg water and subsequently 2×homogenized by means of a microfluidizer. The dispersion is then sterilefiltered above a 0.2 μm filter candle at laminar flow, frozen at −30° C.and dried in vacuum at −35° C. till max. +45° C. The agglomerates areground after drying.

Example 2

White tea extract: 30%

Maltodextrin: 67%

Lipoid P45: 3%

The production corresponds to example 1.

Example 3

Green tea extract: 30%

Maltodextrin: 67%

Lipoid P45: 3%.

The production corresponds to example 1.

Example 4

Hibiscus extract: 30%

Maltodextrin: 67%

Lipoid P 45: 3%.

The production corresponds to example 1.

Example 5

Guarana extract: 30%

Maltodextrin: 67%

Lipoid P 45: 3%

The production corresponds to example 1.

Example 6

Lemon acid: 15%

Vine acid: 10%

Milk acid: 5%

Aerosil: 5%

Maltodextrin: 62%

Lipoid P45: 3%

The production corresponds to example 1.

Example 7

White tea extract: 20%

Maltodextrin: 70%

Lipoid S20: 10%

The production corresponds to example 1.

Example 8

Green tea extract (with 1% caffeine and 5% polyphenols) 40%

Threhalose 59%

Lipoid S75 1%.

The production corresponds to example 1.

Example 9

Guarana extract 20%

Glucose 78%

Phospholipon 80.2%.

The production corresponds to example 1.

Example 10

White tea extract 28%

Mannit 70%

Lipoid S80 2%

The production corresponds to example 1. Cosmetic preparations arepreferred.

Example 11

Production of a Soft Cream

Phase A: 40.0 g SLM 2005 (SLM 2005=Lipoid SLM 2005=base formulationconsisting of hydrated soy lecithin, ethanol, glycerin and middle chaintriglycerides).

Phase B: 82.8 g distilled water, 0.2 g Keltrol CGG-SFT (xanthan rubberproduct with laminar-fluid rheology for transparent solvents,particularly conceived for use as cosmetic and further products for bodycare. Dust free thin fluid powder stable over a large pH array), 1.0 gphospholipon 80H, 1.0 g composition according example 1-5.

Phase C: 36.0 g miglyol, 12.0 g Jojoba oil, 2.0 g Vitamin E-acetate.

Phase D: 12.0 g ethanol, 6.0 g glycerin, 6.0 g hydrolite, 1.0 gpanthenol.

The Phase B is heated up to 60-65° C. till all elements are solved andsubsequently worked into phase A while stirring at 40° C., after thatstirred in phase C and after that phase D is added while stirring ca. 1min. at Ultra-Turax at 40° C. homogenized.

Example 12

Production of a Soft Cream

Phase A: 40.0 g SLM 2005

Phase B: 77.8 g distilled water, 0.2 g keltrol CG-SFT,

Phospholipon 80H

Phase C: 36.0 g miglyol, 12.0 g, Jojoba oil, 2.0 g tocopherolacetat

Phase D: 12.0 g ethanol, 6.0 g glycerin, 6.0 g hydrolyte, 1 g pathenol

Phase E: 5.0 g distilled water, 1.0 g of the composition according toexample 1-5.

The phase B is heated up till 60-65° C. till all components aredissolved and subsequently while stirring at 40° C. worked in to phaseA, then phase C is added while stirring and homogenized. After that at40° C. homogenized phase D is added and while stirring ca. 1 min. atUltra-Turax at 40° C. homogenized.

After that phase E is added while cold stirring.

Example 13

Production of a Lotion

Phase A: 20.0 g SLM 2005

Phase B: 107.6 g distilled water, 0.4 g keltrol CGG-SFT=xanthan Gum (s.o.), 3.0 g, phospholipon 80H, 1.0 g. Composition according example 1-5,1.0 g panthenol.

Phase C: 30.0 g miglyol, 6.0 g Jojoba oil, 2.0 g tocopherolacetate

Phase D: 14.0 g ethanol, 106.0 g glycerin, 6.0 g hydrolyte

The phase B is heated up till 60-65° C. till all components aredissolved and subsequently while stirring at 40° C. worked in to phaseA, then phase C is added and stirred homogenous. After that phase D isadded and while stirring ca. 1 min. at an Ultra-Turax at 40° C.homogenized.

Example 14

Production of a Lotion

Phase A: 20.0 g SLM 2005

Phase B: 97.6 g distilled water, 0.4 g keltrol CGG-SFT, 3.0 gphospholipon 80H=hydrated phospholipid with ca. 80% phosphatidylcholine,1.0 g composition according example 1-5, 1.0 g panthenol.

Phase C: 30.0 g miglyol=fatty acid ester, 6.0 g Jojoba oil, 1.0 gtocopherolacetat, 14.0 g ethanol, 10.0 g glycerin, 6.0 g hydrolite.

Phase D: 10.0 g distilled water, 1.0 g of the composition accordingexample 1-5.

The phase B is heated up till 60-65° C. till all components aredissolved and subsequently while stirring at 40° C. worked in to phaseA, then phase C is added and stirred homogenous. After that phase D isadded and while stirring ca. 1 min. at an Ultra-Turax at 40° C.homogenized.

Example 15

Cream

Phase A: 18.0 g miglyol 812, 9.0 g tegosoft DC, 10.0 g Avocado oil, 6.0g lanette 18, 2.0 g Tegin M, 0.2 g stearin acid, 1.0 g tocopherolacetat

Phase B: 2.0 g tegoCare Cg 90; 6.0 g glycerin, 1.0 g panthenol, 0.4 gallatoin, 132.2 g water.

Phase C: 1.0 g of the composition according example 1-5, 9.0 g water

Phase D: 0.4 g preserving agent.

The phases A and B are respectively heated up till 80 C. Phase B isworked into phase A while stirring and subsequently post-homogenized 1min. by an Ultra-Turax.

What is claimed is:
 1. A composition consisting of: a) 0.5-40 weight %vegetable extract; b) 30-90 weight % maltodextrin; and c) 0.5-30 weight% phospholipid including 40-80% of phosphatidylcholine.
 2. Thecomposition according to claim 1, consisting of: a) 18-35 weight % ofthe vegetable extract; b) 40-80 weight % of the maltodextrin; and c)1-25 weight % of the phospholipid.
 3. The composition according to claim1, consisting of: a) 28-32 weight % of the vegetable extract; b) 60-70weight % of the maltodextrin; and c) 2-8 weight % of the phospholipid.4. The composition according to claim 1, consisting of: a) 30 weight %of the vegetable extract; b) 67 weight % of the maltodextrin; and c) 3weight % of the phospholipid.
 5. The composition according to claim 1,wherein the composition is provided in a dry form as a powder or asgranules.
 6. The composition according to claim 5, wherein the dry formis a lyophilisate.
 7. The composition according to claim 6, wherein thecomposition spontaneously forms liposomes when redispersing.
 8. Thecomposition according to claim 1, wherein the vegetable extract isselected from the group consisting of Aloe, Rooibos, Guarana, white tea,green tea, black tea, Hibiskus, Nettle, Rofippa amphibia, water cress,horse tail, field horsetail, chamomile, Centella asiatica, Gingko,Ginseng, Cranberry, olive, pomegranate or mixtures thereof.
 9. A methodfor the production of a composition according to claim 1, wherein thevegetable extract, the maltodextrin and the phospholipid are dispersedand homogenized in water, then sterile filtered and subsequently driedat −30° C. to +45° C., and the dried product is ground to a grain sizewith an orifice diameter of 0.5-1.5 mm.
 10. The composition according toclaim 1 as a cosmetic, dietary or pharmaceutical formulation.